US8476235B2ActiveUtilityPatentIndex 60
Crystalline D-isoglutamyl-D-tryptophan and the mono ammonium salt of D-isoglutamyl-D-tryptophan
Est. expiryNov 28, 2026(~0.4 yrs left)· nominal 20-yr term from priority
A61P 37/06A61P 37/00A61P 17/06C07K 5/0215A61K 38/00A61K 38/05C07K 1/107C07K 1/30C07K 5/06
60
PatentIndex Score
1
Cited by
22
References
24
Claims
Abstract
A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.
Claims
exact text as granted — not AI-modifiedThe invention claimed is:
1. Crystalline H-D-iGlu-D-Trp-OH, ammonium salt (1:1) characterized by the x-ray powder diffraction pattern as illustrated in FIG. 2 .
2. Crystalline H-D-iGlu-D-Trp-OH, ammonium salt (1:1) characterized by the following X-ray powder diffraction pattern expressed in terms of inter-planar distances d, Bragg's angle 2 theta, and relative intensity (expressed as a percentage with respect to the most intense ray):
Angle [°2 theta]
d-value [Å]
Rel. Int [%]
9.29
9.517
4.1
12.19
7.258
4.5
13.93
6.354
76.2
15.17
5.837
27.4
16.49
5.371
9.8
17.18
5.157
3
18.56
4.778
31.6
18.88
4.696
10.5
20.02
4.431
100
22.28
3.986
3
23.31
3.814
4.6
23.66
3.757
9.8
24.03
3.7
52.9
24.37
3.649
26.3
25.07
3.549
11.4
25.61
3.475
5.6
25.96
3.43
5
27.62
3.227
29.7
28.12
3.17
55.7
28.49
3.131
12.2
29.52
3.023
23.1
30.27
2.951
3.7
30.64
2.915
7.9
31.31
2.854
11.8
31.7
2.821
29.6
32.16
2.781
19.2
32.81
2.728
16
33.78
2.652
7.4
34.14
2.625
5.1
35.76
2.509
16
36.94
2.431
11.6
37.58
2.391
25.6
38.03
2.364
12.5
39.22
2.295
1.9.
3. Crystalline H-D-iGlu-D-Trp-OH, ammonium salt (1:1) having an X-ray powder diffraction pattern comprising peaks at 2θ angles of approximately 13.93, 20.02, 24.03 and 28.12 degrees.
4. Crystalline H-D-iGlu-D-Trp-OH, ammonium salt (1:1) having an X-ray powder diffraction pattern comprising peaks at approximately 9.29, 12.19, 13.93, 15.17, 16.49, 17.18, 18.56, 18.88, 20.02, 22.28, 23.31, 23.66, 24.03, 24.37, 25.07, 25.61, 25.96, 27.62, 28.12, 28.49, 29,52, 30.27, 30.64, 31.31, 31.70, 32.16, 32.81, 33.78, 34.14, 35.76, 36.94, 37.58, 38.03 and 39.22 degrees 2θ.
5. The crystalline salt of claim 3 having an X-ray powder diffraction pattern comprising peaks at 2θ angles of approximately 13.93, 15.17, 18.56, 20.02, 24.03, 24.37, 27.62, 28.12, 31.7 and 37.58 degrees.
6. Crystalline H-D-iGlu-D-Trp-OH, ammonium salt (1:1) characterized by the infrared absorption spectrum as illustrated in FIG. 4 .
7. A pharmaceutical composition comprising the crystalline salt of claim 1 and at least one pharmaceutically acceptable excipient.
8. A pharmaceutical composition comprising the crystalline salt of claim 2 and at least one pharmaceutically acceptable excipient.
9. A pharmaceutical composition comprising the crystalline salt of claim 3 and at least one pharmaceutically acceptable excipient.
10. A pharmaceutical composition comprising the crystalline salt of claim 4 and at least one pharmaceutically acceptable excipient.
11. A pharmaceutical composition comprising the crystalline salt of claim 5 and at least one pharmaceutically acceptable excipient.
12. A pharmaceutical composition comprising the crystalline salt of claim 6 and at least one pharmaceutically acceptable excipient.
13. A method of treating psoriasis comprising administering an effective amount of the crystalline salt of claim 1 or the pharmaceutical composition of claim 7 to a subject in need thereof.
14. A method of treating psoriasis comprising administering an effective amount of the crystalline salt of claim 2 or the pharmaceutical composition of claim 8 to a subject in need thereof.
15. A method of treating psoriasis comprising administering an effective amount of the crystalline salt of claim 3 or the pharmaceutical composition of claim 9 to a subject in need thereof.
16. A method of treating psoriasis comprising administering an effective amount of the crystalline salt of claim 4 or the pharmaceutical composition of claim 10 to a subject in need thereof.
17. A method of treating psoriasis comprising administering an effective amount of the crystalline salt of claim 5 or the pharmaceutical composition of claim 11 to a subject in need thereof.
18. A method of treating psoriasis comprising administering an effective amount of the crystalline salt of claim 6 or the pharmaceutical composition of claim 12 to a subject in need thereof.
19. A method of selectively inhibiting proliferation of bone marrow cells in a subject in need thereof comprising administering an effective amount of the crystalline salt of claim 1 or the pharmaceutical composition of claim 7 to a subject in need thereof.
20. A method of selectively inhibiting proliferation of bone marrow cells in a subject in need thereof comprising administering an effective amount of the crystalline salt of claim 2 or the pharmaceutical composition of claim 8 to a subject in need thereof.
21. A method of selectively inhibiting proliferation of bone marrow cells in a subject in need thereof comprising administering an effective amount of the crystalline salt of claim 3 or the pharmaceutical composition of claim 8 to a subject in need thereof.
22. A method of selectively inhibiting proliferation of bone marrow cells in a subject in need thereof comprising administering an effective amount of the crystalline salt of claim 4 or the pharmaceutical composition of claim 10 to a subject in need thereof.
23. A method of selectively inhibiting proliferation of bone marrow cells in a subject in need thereof comprising administering an effective amount of the crystalline salt of claim 5 or the pharmaceutical composition of claim 11 to a subject in need thereof.
24. A method of selectively inhibiting proliferation of bone marrow cells in a subject in need thereof comprising administering an effective amount of the crystalline salt of claim 6 or the pharmaceutical composition of claim 12 to a subject in need thereof.Cited by (0)
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